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1. WO2008043911 - DENDRITIC CHELATED COMPOUNDS, METHODS FOR MAKING THE SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

Publication Number WO/2008/043911
Publication Date 17.04.2008
International Application No. PCT/FR2007/001645
International Filing Date 09.10.2007
IPC
A61K 49/10 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
49Preparations for testing in vivo
06Nuclear magnetic resonance (NMR) contrast preparations; Magnetic resonance imaging (MRI) contrast preparations
08characterised by the carrier
10Organic compounds
A61K 49/12 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
49Preparations for testing in vivo
06Nuclear magnetic resonance (NMR) contrast preparations; Magnetic resonance imaging (MRI) contrast preparations
08characterised by the carrier
10Organic compounds
12Macromolecular compounds
C07C 225/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
225Compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly-bound oxygen atoms not being part of a -CHO group, e.g. amino ketones
02having amino groups bound to acyclic carbon atoms of the carbon skeleton
04the carbon skeleton being saturated
06and acyclic
C07C 233/18 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
233Carboxylic acid amides
01having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
16having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
17with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
18having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
C07C 237/08 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
237Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
02having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
04the carbon skeleton being acyclic and saturated
08having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
C07D 215/26 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
215Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
16with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
20Oxygen atoms
24attached in position 8
26Alcohols; Ethers thereof
CPC
A61K 49/124
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
49Preparations for testing in vivo
06Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
08characterised by the carrier
10Organic compounds
12Macromolecular compounds
124dendrimers, dendrons, hyperbranched compounds
A61K 51/0478
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51Preparations containing radioactive substances for use in therapy or testing in vivo
02characterised by the carrier ; , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
04Organic compounds
0474complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group
0478complexes from non-cyclic ligands, e.g. EDTA, MAG3
C07C 229/16
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
229Compounds containing amino and carboxyl groups bound to the same carbon skeleton
02having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
04the carbon skeleton being acyclic and saturated
06having only one amino and one carboxyl group bound to the carbon skeleton
10the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
16to carbon atoms of hydrocarbon radicals substituted by amino or carboxyl groups, e.g. ethylenediamine-tetra-acetic acid, iminodiacetic acids
C07C 229/76
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
229Compounds containing amino and carboxyl groups bound to the same carbon skeleton
76Metal complexes of amino carboxylic acids
C07C 237/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
237Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
02having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
04the carbon skeleton being acyclic and saturated
08having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
C07C 237/22
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
237Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
02having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
22having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
Applicants
  • CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE [FR]/[FR] (AllExceptUS)
  • UNIVERSITE LOUIS PASTEUR [FR]/[FR] (AllExceptUS)
  • FELDER-FLESCH, Delphine [FR]/[FR] (UsOnly)
  • STEIBEL, Jérôme [FR]/[FR] (UsOnly)
  • BERTIN, Annabelle [FR]/[FR] (UsOnly)
Inventors
  • FELDER-FLESCH, Delphine
  • STEIBEL, Jérôme
  • BERTIN, Annabelle
Agents
  • NOËL, Chantal
Priority Data
06 0883609.10.2006FR
Publication Language French (FR)
Filing Language French (FR)
Designated States
Title
(EN) DENDRITIC CHELATED COMPOUNDS, METHODS FOR MAKING THE SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
(FR) COMPLEXES CHELATES DENDRITIQUES, LEURS PROCEDES DE FABRICATION ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT
Abstract
(EN)
The invention relates to dendritic chelated compounds, to methods for producing the same and to pharmaceutical compositions containing the same. The dendritic chelated complexes of the present invention have the following formula (I): [[MC]-En-[D]m-X1p1X2p2X3p3 X4p4]z- z B+ (I), where m is a magnetic or scintigraphic marker, C is a chelating agent of the marker M, E is a spacer, n = 0 or 1, D is compound capable of forming a dendritic structure, m is an integer equal to 1 or 2 or 4, X1 is a group increasing the complex lipophily, p1 is an integer from 0 to 12, X2 is a group increasing the complex specificity for a particular organ, p2 is an integer equal to 1 or 2 or 4, X3 is a group having a therapeutic activity, p3 is an integer equal to 0, 1, 2 or 4, X4 is a CH3 group, p4 is an integer from 0 to 12, B is a counter-ion, z is an integer equal to 0, 1, 2, 3 or 4. The invention can be used in the field of pharmacy, more precisely in medical imaging.
(FR)
L'invention concerne des complexes chélatés dendritiques, leurs procédés de fabrication et les compositions pharmaceutiques les contenant. Les complexes chélatés dendritiques selon l'invention ont la formule I suivante : [[MC]-En-[D]m-X1p1X2p2X3p3 X4p4]z- z B+ (I), dans laquelle M est un marqueur magnétique ou scintigraphique, C est un agent chélatant du marqueur magnétique M, E est un espaceur, n = 0 ou 1, D est un composé apte à former une structure dendritique, m est un entier valant 1 ou 2 ou 4, X1 est un groupement augmentant la lipophilie du complexe, p1 est un entier valant de 0 à 12 inclus, X2 est un groupement augmentant la spécificité du complexe pour un organe particulier, p2 est un entier valant 0, 1, 2, ou 4 inclus, X3 est un groupement ayant une activité thérapeutique, p3 est un entier valant 0, 1, 2, ou 4 inclus, X4 est un groupement CH3, p4 est un entier valant de 0 à 12 inclus, B est un contre ion, z est un entier valant 0, 1, 2, 3 ou 4. L'invention trouve application dans le domaine pharmaceutique, plus particulièrement dans le domaine de l'imagerie médicale.
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